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Pb-212-CA012 (also known as 212Pb-CA012 or 212Pb-PSMA-CA012) is a prostate-specific membrane antigen (PSMA)-targeted radiopharmaceutical developed by the German Cancer Research Center (DKFZ) and Heidelberg University. It consists of a Glu-urea-based PSMA-targeting ligand conjugated to the chelator DO3AM via an Amcha linker, radiolabeled with the alpha-emitting radionuclide lead-212 (Pb-212). Lead-212 acts as an in vivo generator of the potent alpha-emitter bismuth-212, delivering highly localized, cytotoxic alpha radiation to PSMA-expressing prostate cancer cells while minimizing damage to surrounding healthy tissues. Pb-212-CA012 is being investigated for the treatment of metastatic castration-resistant prostate cancer (mCRPC), with its elementally matched imaging analogue, Pb-203-CA012, utilized for diagnostic SPECT imaging and dosimetry.
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